VEGF Inhibitor, V1

An NRP-1-binding heptapeptide whose target was initially mistaken as VEGFR2/KDR/Flk-1 due to its binding activity to a CHO-KDR culture that was later shown to express primarily NRP-1 and little KDR. V1/A7R specifically competes against VEGF₁₆₅ binding to recombinant NRP-1 in cell-free binding assays (IC₅₀ = 60 µM), while exhibiting no activity against the interaction between NRP-1 and heparin or VEGF₁₆₅ binding to KDR, VEGFR1/Flt-1, and heparin. V1/A7R is demonstrated to inhibit VEGF-dependent angiogenesis activity in HMVEC (IC₅₀ = 0.3 µM) and HUVEC cultures in vitro, as well as in a rabbit corneal neovascularization model and in mice bearing MDA-MB-231-derived tumor in vivo.

An NRP-1-binding heptapeptide whose target was initially mistaken as VEGFR2/KDR/Flk-1 due to its binding activity to a CHO-KDR culture that was later shown to express primarily NRP-1 and little KDR. V1/A7R specifically competes against VEGF₁₆₅ binding to recombinant NRP-1 in cell-free binding assays (IC₅₀ = 60 µM), while exhibiting no activity against the interaction between NRP-1 and heparin or VEGF₁₆₅ binding to KDR, VEGFR1/Flt-1, and heparin. V1/A7R is demonstrated to inhibit VEGF-dependent angiogenesis activity in HMVEC (IC₅₀ = 0.3 µM) and HUVEC cultures in vitro, as well as in a rabbit corneal neovascularization model and in mice bearing MDA-MB-231-derived tumor in vivo.

Cell permeable: no

Primary Target
Specifically competes against VEGF165 binding to recombinant NRP-1

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 60 µM for specifically competes against VEGF165 binding to recombinant NRP-1 in cell-free binding assays

Packaged under inert gas

Toxicity: Standard Handling (A)

H-Ala-Thr-Trp-Leu-Pro-Pro-Arg-OH

Starzec, A., et al. 2006. Life Sci.79, 2370.
Binetruy-Tournaire, R., et al. 2000. EMBO J.19, 1525.

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